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首页> 外文期刊>The Open Drug Delivery Journal >Effect of 5-Fluorouracil Pretreatment on the In Vitro Drug Release from Colon-Targeted Guar Gum Matrix Tablets
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Effect of 5-Fluorouracil Pretreatment on the In Vitro Drug Release from Colon-Targeted Guar Gum Matrix Tablets

机译：5-氟尿嘧啶预处理对结肠靶向瓜尔胶基质片剂体外药物释放的影响

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The aim of the investigation was to assess the effect of oral 5-flourouracil pre-treatment on the in vitro drug releasefrom a model colon-targeted guar gum matrix tablet formulation of mebendazole. Guar gum matrix tablets of mebendazolewere subjected to in vitro drug release studies in simulated colonic fluids (4%w/v of rat caecal contents) obtainedafter oral treatment of rats either with varying doses of 5-fluorouracil (0.3, 1, 3 or 6 mg kg-1 once daily for 5 days)and 1 ml of 2%w/v of guar gum dispersion or with 1 ml of 2%w/v of guar gum dispersion alone (control study) aftercompleting the dissolution study in 0.1 M HCl (2 h) and pH 7.4 Sorensen’s phosphate buffer (3 h). The mebendazole tabletsdisintegrated in the presence of simulated colonic fluids releasing about 97% of the drug (control study) at the end of24 h. However, the release of mebendazole decreased when drug release studies were carried out in caecal contents of ratspretreated with both 5-fluorouracil and guar gum dispersion. The release of mebendazole significantly decreased whenpretreated with 1, 3 or 6 mg kg-1 dose levels of 5-fluorouracil (oral). However, there was no significant effect of 5-fluorouracil on the release of mebendazole when pretreated at a dose level of 0.3 mg kg-1 (oral). It was concluded thatmultiple administration of 5-fluorouracil at a dose of 0.3 mg kg-1 did not affect the drug release from colon-targeted guargum matrix tablets.
机译：该研究的目的是评估口服5-氟尿嘧啶预处理对从模型结肠靶向瓜巴胶基质的甲苯咪唑的体外药物释放的影响。口服不同剂量的5-氟尿嘧啶（0.3、1、3或6 mg）口服治疗大鼠后，在模拟结肠液（大鼠盲肠内容物的4％w / v）中对甲苯达唑的瓜尔胶基质片剂进行了体外药物释放研究每天1 kg-1，持续5天）和1 ml 2％w / v瓜尔胶分散液，或仅含1ml 2％w / v瓜尔胶分散液（对照研究），以0.1 M HCl（ 2 h）和pH 7.4的Sorensen磷酸盐缓冲液（3 h）。在模拟结肠液存在下，甲苯苯达唑片崩解，在24小时结束时释放约97％的药物（对照研究）。然而，当对接受5-氟尿嘧啶和瓜尔胶分散液预处理的大鼠的盲肠内容物进行药物释放研究时，甲苯达唑的释放降低。用1、3或6 mg kg-1剂量的5-氟尿嘧啶（口服）预处理时，甲苯达唑的释放显着降低。但是，当以0.3 mg kg-1（口服）的剂量进行预处理时，5-氟尿嘧啶对甲苯达唑的释放没有显着影响。结论是，以0.3 mg kg-1的剂量多次施用5-氟尿嘧啶并不会影响靶向结肠的Guargum基质片剂的药物释放。

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